Anticancer agent 44

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Anticancer agent 44 (compound 2a) is a potent anticancer agent. Anticancer agent 44 shows cytotoxicity activity in cancer cells. Anticancer agent 44 induces apoptosis. Anticancer agent 44 shows low toxicity towards activated lymphocytes of human blood.

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Anticancer agent 44 Chemical Structure

CAS No. : 2770943-86-5

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Biological Activity
Purity & Documentation
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	1.63 μM Compound: 2a	Anticancer activity against human 786-0 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human 786-0 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
A549	GI₅₀	63.9 μM Compound: 2a	Anticancer activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
ACHN	GI₅₀	1.34 μM Compound: 2a	Anticancer activity against human ACHN cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human ACHN cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
BT-549	GI₅₀	1.75 μM Compound: 2a	Anticancer activity against human BT-549 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human BT-549 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
CAKI-1	GI₅₀	1.13 μM Compound: 2a	Anticancer activity against human CAKI-1 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human CAKI-1 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
CCRF-CEM	GI₅₀	0.486 μM Compound: 2a	Anticancer activity against human CCRF-CEM cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human CCRF-CEM cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
COLO 205	GI₅₀	1.4 μM Compound: 2a	Anticancer activity against human COLO 205 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human COLO 205 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
DU-145	GI₅₀	2.09 μM Compound: 2a	Anticancer activity against human DU-145 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human DU-145 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
EKVX	GI₅₀	3.11 μM Compound: 2a	Anticancer activity against human EKVX cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human EKVX cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HaCaT	GI₅₀	> 100 μM Compound: 2a	Cytotoxicity against human HaCaT cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Cytotoxicity against human HaCaT cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
HCC 2998	GI₅₀	1.59 μM Compound: 2a	Anticancer activity against human HCC 2998 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HCC 2998 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HCT-116	GI₅₀	1.35 μM Compound: 2a	Anticancer activity against human HCT-116 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HCT-116 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HCT-116	GI₅₀	9.18 μM Compound: 2a	Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
HCT-15	GI₅₀	0.599 μM Compound: 2a	Anticancer activity against human HCT-15 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HCT-15 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HeLa	GI₅₀	6.65 μM Compound: 2a	Anticancer activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human HeLa cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
HL-60	GI₅₀	1.45 μM Compound: 2a	Anticancer activity against human HL-60 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HL-60 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HOP-62	GI₅₀	1.73 μM Compound: 2a	Anticancer activity against human HOP-62 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HOP-62 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HOP-92	GI₅₀	2.58 μM Compound: 2a	Anticancer activity against human HOP-92 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HOP-92 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
Hs-578T	GI₅₀	1.8 μM Compound: 2a	Anticancer activity against human Hs-578T cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human Hs-578T cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
HT-29	GI₅₀	0.632 μM Compound: 2a	Anticancer activity against human HT-29 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human HT-29 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
IGROV-1	GI₅₀	1.03 μM Compound: 2a	Anticancer activity against human IGROV-1 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human IGROV-1 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
Jurkat	GI₅₀	3.4 μM Compound: 2a	Anticancer activity against human Jurkat cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human Jurkat cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
K562	GI₅₀	0.692 μM Compound: 2a	Anticancer activity against human K562 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human K562 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
KB 3-1	GI₅₀	70.3 μM Compound: 2a	Anticancer activity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
KM12	GI₅₀	1.96 μM Compound: 2a	Anticancer activity against human KM12 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human KM12 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
Lymphocyte	GI₅₀	28.9 μM Compound: 2a	Cytotoxicity against mitogen activated human peripheral blood lymphocytes assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against mitogen activated human peripheral blood lymphocytes assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35533562]
Lymphocyte	GI₅₀	36.8 μM Compound: 2a	Cytotoxicity against mitogen activated human peripheral blood lymphocytes assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against mitogen activated human peripheral blood lymphocytes assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 35533562]
M14	GI₅₀	2.11 μM Compound: 2a	Anticancer activity against human M14 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human M14 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
Malme-3M	GI₅₀	3.09 μM Compound: 2a	Anticancer activity against human Malme-3M cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human Malme-3M cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
MCF7	GI₅₀	1.38 μM Compound: 2a	Anticancer activity against human MCF7 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human MCF7 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
MCF7	GI₅₀	7.95 μM Compound: 2a	Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
MDA-MB-231	GI₅₀	3.75 μM Compound: 2a	Anticancer activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
MDA-MB-231	GI₅₀	6.45 μM Compound: 2a	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
MDA-MB-435	GI₅₀	1.65 μM Compound: 2a	Anticancer activity against human MDA-MB-435 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human MDA-MB-435 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
MDA-MB-468	GI₅₀	1.33 μM Compound: 2a	Anticancer activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
MOLT-4	GI₅₀	0.596 μM Compound: 2a	Anticancer activity against human MOLT-4 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human MOLT-4 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI/ADR-RES	GI₅₀	1.01 μM Compound: 2a	Anticancer activity against human NCI/ADR-RES cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI/ADR-RES cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI-H226	GI₅₀	1.92 μM Compound: 2a	Anticancer activity against human NCI-H226 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI-H226 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI-H23	GI₅₀	1.64 μM Compound: 2a	Anticancer activity against human NCI-H23 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI-H23 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI-H322M	GI₅₀	3 μM Compound: 2a	Anticancer activity against human NCI-H322M cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI-H322M cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI-H460	GI₅₀	3.3 μM Compound: 2a	Anticancer activity against human NCI-H460 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI-H460 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
NCI-H522	GI₅₀	1.73 μM Compound: 2a	Anticancer activity against human NCI-H522 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human NCI-H522 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
OVCAR-3	GI₅₀	0.721 μM Compound: 2a	Anticancer activity against human OVCAR-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human OVCAR-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
OVCAR-4	GI₅₀	5.55 μM Compound: 2a	Anticancer activity against human OVCAR-4 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human OVCAR-4 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
OVCAR-5	GI₅₀	2.04 μM Compound: 2a	Anticancer activity against human OVCAR-5 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human OVCAR-5 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
OVCAR-8	GI₅₀	0.832 μM Compound: 2a	Anticancer activity against human OVCAR-8 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human OVCAR-8 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
PC-3	GI₅₀	1.34 μM Compound: 2a	Anticancer activity against human PC-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human PC-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
RPMI-8226	GI₅₀	0.303 μM Compound: 2a	Anticancer activity against human RPMI-8226 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human RPMI-8226 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
RXF 393	GI₅₀	1.26 μM Compound: 2a	Anticancer activity against human RXF 393 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human RXF 393 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SF-268	GI₅₀	3.07 μM Compound: 2a	Anticancer activity against human SF-268 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SF-268 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SF-295	GI₅₀	1.4 μM Compound: 2a	Anticancer activity against human SF-295 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SF-295 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SF-539	GI₅₀	1.69 μM Compound: 2a	Anticancer activity against human SF-539 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SF-539 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SK-MEL-2	GI₅₀	3.12 μM Compound: 2a	Anticancer activity against human SK-MEL-2 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SK-MEL-2 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SK-MEL-28	GI₅₀	1.71 μM Compound: 2a	Anticancer activity against human SK-MEL-28 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SK-MEL-28 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SK-MEL-5	GI₅₀	1.95 μM Compound: 2a	Anticancer activity against human SK-MEL-5 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SK-MEL-5 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SK-OV-3	GI₅₀	3.56 μM Compound: 2a	Anticancer activity against human SK-OV-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SK-OV-3 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SK-OV-3	GI₅₀	65.9 μM Compound: 2a	Anticancer activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
SN12C	GI₅₀	1.69 μM Compound: 2a	Anticancer activity against human SN12C cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SN12C cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SNB-19	GI₅₀	1.17 μM Compound: 2a	Anticancer activity against human SNB-19 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SNB-19 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SR	GI₅₀	0.544 μM Compound: 2a	Anticancer activity against human SR cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SR cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
SW-620	GI₅₀	0.508 μM Compound: 2a	Anticancer activity against human SW-620 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human SW-620 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
T47D	GI₅₀	2.03 μM Compound: 2a	Anticancer activity against human T47D cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human T47D cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
TK-10	GI₅₀	2.79 μM Compound: 2a	Anticancer activity against human TK-10 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human TK-10 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
U-251	GI₅₀	0.477 μM Compound: 2a	Anticancer activity against human U-251 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human U-251 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
U-251	GI₅₀	8.93 μM Compound: 2a	Anticancer activity against human U-251 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Anticancer activity against human U-251 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35533562]
UACC-257	GI₅₀	2.92 μM Compound: 2a	Anticancer activity against human UACC-257 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human UACC-257 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
UACC-62	GI₅₀	1.77 μM Compound: 2a	Anticancer activity against human UACC-62 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human UACC-62 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]
UO-31	GI₅₀	1.07 μM Compound: 2a	Anticancer activity against human UO-31 cells assessed as growth inhibition incubated for 48 hrs by SRB assay Anticancer activity against human UO-31 cells assessed as growth inhibition incubated for 48 hrs by SRB assay	[PMID: 35533562]

In Vitro

Anticancer agent 44 (compound 2a) (0-100 µM; 72 h) shows antitumor activity with GI₅₀s of 3.40, 63.90, 7.95, 6.45, 70.30, 6.65, 9.18, 6.00, 8.93, 65.90, >100 µM for Jurkat, A549, MCF-7, MDA-MB-231, KB3-1, HeLa, HCT-116, HCT-116 p53-/-, U251, SK-OV-3, HaCaT cells, respectively^[1].
Anticancer agent 44 (1.5 µM; 24 h) induces apoptosis by increases the expression of caspase 3, Bax and decreases the amount of anti-apoptotic Bcl-2 protein^[1].
Anticancer agent 44 (0-2 µM; 24, 48 h) shows low toxicity towards normal human keratinocytes of HaCaT line and mitogen-activated lymphocytes of peripheral blood of healthy human donor^[1].
Anticancer agent 44 dose not induce significant DNA damage and changes in morphology of mitogen-activated lymphocytes of peripheral blood of healthy donor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

534.39

Formula

C₂₂H₁₃Cl₂N₃O₅S₂

CAS No.

2770943-86-5

SMILES

O=C1CC(C(N1C2=CC=C(C=C2)Cl)=O)N3C(/C(SC3=S)=C/C(Cl)=C/C4=CC=C(C=C4)[N+]([O-])=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Nataliya Finiuk, et al. Novel hybrid pyrrolidinedione-thiazolidinones as potential anticancer agents: Synthesis and biological evaluation. Eur J Med Chem. 2022 May 2;238:114422. [Content Brief]

[2]. Finiuk N, et al. Novel hybrid pyrrolidinedione-thiazolidinones as potential anticancer agents: Synthesis and biological evaluation. Eur J Med Chem. 2022 May 2;238:114422.