anticancer agent 13

Anticancer agent 13 is a compound derived from dicarboxylic acids and amines, developed for use as an anticancer agent.

Compound Rh1 (Anticancer agent 132) acts as an inducer of apoptosis and autophagy, exhibiting both antitumor and antimetastatic activities. It also arrests the cell cycle and inhibits cell proliferation [1].

Compound Rh2 (Anticancer agent 133) is a cytotoxic and antimetastatic agent that induces cell cycle arrest, apoptosis, and autophagy. Additionally, it suppresses cell metastasis through the inhibition of EGFR expression, which is mediated by FAK-regulated integrin β1 [1].

Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM), exhibits an IC50 value of 3.38 μM against human dermal fibroblasts (HDF) and binds to Heat shock protein 90 (Hsp90) with a dissociation constant (Kd) of 3.86 μM, demonstrating its apoptosis-inducing capabilities [1].

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI ADR-RES, 786-O, A549 ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

Anticancer agent 130 (compound 8d) significantly induces apoptosis in A549 cells [1].

Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist that blocks AR nuclear translocation and inhibits AR AR-V7 heterodimerization to suppress downstream gene transcription, demonstrating strong efficacy in prostate cancer xenograft models [1].

Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2 M cell cycle arrest and apoptosis. It increases levels of cleaved PARP, and caspases 3 and 7, making it useful in cancer research [1].

HCT-116-IN-1, a γ-lactam-fused pyridone derivative, demonstrates significant anticancer properties with cytotoxicity towards HCT116 cells at an IC50 value of 5.59 μM [1].

Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability. It halts the cell cycle at the G2 M phase and induces apoptosis [1].

Anticancer agent 237 (compound 13) (48 h) induces apoptosis and cell cycle arrest at S and G2 M phases in HCT-116 and MCF-7 cells.