antiproliferative

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

Antiproliferative agent-22 is an anticancer compound that shows antiproliferative activity on MCF-7, MDA-MB-231, and MDA-MB-468 cells.Antiproliferative agent-22 is used in cancer research.

Antiproliferative agent-13 is a compound with antiproliferative activity.

Antiproliferative agent-16 (Antiproliferative agent-16) is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells).

Antiproliferative agent-15 is a reagent with anticancer activity. Antiproliferative agent-15 showed antiproliferative activity against human colon cancer (HCT116 and HCT15) and brain cancer (LN-229 and GBM-10).

Antiproliferative agent-60 (compound 8c), an 11-Azaartemisinin derivative, exhibits outstanding anticancer activity. It demonstrates tumor selectivity up to 32 times higher when compared to normal Hek293 cells. The IC50 values for Antiproliferative agent-60 are 7.7 μM for epidermoid carcinoma (KB), 42.5 μM for HepG2, and 15.5 μM for A549 cells.

Antiproliferative agent-26 (compound 4g) shows broad-spectrum activity against leukemia, CNS cancers, melanoma, renal, and breast cancers at 10 μM, inhibits colony formation, induces G1 phase cell cycle arrest at 5 μM, and causes S phase cell cycle arrest at 25 μM [1].

Antiproliferative Agent-39 (Compound 12) effectively inhibits the proliferation of various cancer cell lines, including A549, SNU-638, Col2, HT1080, and MCF-7, with respective IC50 values of 11, 25, 14, 11, and 6.3 μM [1].

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound exhibiting antiproliferative activity. It inhibits cancer cell lines HCT116, MCF-7, H460, and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50 values of 0.5 μM, 2 μM, 0.7 μM, and 3.5 μM, respectively.

Antiproliferative agent-3 (comp 4) exhibits potent growth inhibitory effects against MCF-7 cells with an IC50 of 0.19 nM [1].

Antiproliferative Agent-27 (Compound 11) is a notable antiproliferative agent that markedly diminishes tumor cell colony formation and induces apoptosis, demonstrating potential for utilization in cancer research [1].

Antiproliferative agent-4 showed good anti-proliferative effects on some cancer cells. antiproliferative agent-4 inhibited tumour growth in nude mice and showed low toxicity. antiproliferative agent-4 reduced the mitochondrial membrane potential of EC109 cells and increased Antiproliferative agent-4 reduced the mitochondrial membrane potential of EC109 cells and increased the apoptosis rate and ROS level.

Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2 M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.

Antiproliferative Agent-34 (Compound A14), a multitarget kinase inhibitor, demonstrates IC50 values of 177 nM for EGFR L858R T790M and 1567 nM for EGFR WT. Additionally, it inhibits JAK2, ROS1, FLT3, FLT4, and PDGFRα with respective IC50s of 30.93 nM, 106.90 nM, 108.00 nM, 226.60 nM, and 42.53 nM. In normoxic conditions, it suppresses the proliferation of H1975 and HCC827 cells with IC50 values below 40 nM, while under hypoxic conditions, its potency increases 4-6 fold, yielding IC50 values less than 10 nM [1].

Antiproliferative agent-5 (compound 4o) irreversibly and significantly inhibits the proliferation of gastric cancer cells, blocks the cell cycle in the G2 M phase, induces ROS accumulation, and activates cellular autophagy. Antiproliferative agent-5 can be used in anti-cancer research.

Antiproliferative Agent-42 (Compound 7m), a dihydrodipyrrolo compound, exhibits antiproliferative activity against the Panc-1 cell line, with an IC 50 of 12.54 μM [1].

Antiproliferative agent-36 is a broad-spectrum anticancer benzothiazolylhydrazone-derived compound that inhibits cell proliferation.