Antiproliferative

5-fluorouridine is also known as FUrd, 5-Fluorouracil 1-beta-D-ribofuranoside, 5-Fur, or 5-Fluoro-uridine. 5-fluorouridine is a solid. This compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar. 5-fluorouridine is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparison studies with fluorouracil and thymine analogs.

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.

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.

Dipyrithione appears to have novel cytotoxicity and potent broad-spectrum antitumor activity

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.

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

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.

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

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

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)

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-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-13 is a compound with antiproliferative activity.

Antiproliferative Agent-58 (compound 8nj) is an effective antiproliferative agent that exhibits activity under both normoxic and hypoxic conditions.

Antiproliferative agent-56 (Compound 31) is an antimalarial agent that inhibits the Pf3D7 strain of the malaria parasite Plasmodium falciparum with an IC50 of >12.5 (48h) and 0.03 μM (98h), displaying slow-acting characteristics.

Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor that suppresses VEGF secretion in SiHa cells under hypoxic conditions without inducing cytotoxicity (IC50=0.68 μM). It modulates the PI3K AKT mTOR and MAPK signaling pathways in tumor cells, thereby inhibiting the expression of HIF-1α and VEGF within tumor tissues.

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-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-63 (compound 4d) is a cyclic analog of cannabidiol that acts as an anticancer agent. It demonstrates favorable activity against breast and colorectal cancer. Moreover, this compound can arrest the cell cycle in the G1 phase and induce apoptosis through the mitochondrial pathway in breast cancer cell lines.

Antiproliferative agent-64 (Compound 76) functions as an inhibitor of the eukaryotic translation initiation factor 4E (eIF4E) and disrupts the secondary structure of mRNA, thereby hindering protein translation. It inhibits the 5' untranslated region (5'UTR) of c-Myc with an EC50 of 1.2 nM and the 5'UTR of tubulin with an EC50 of 40 nM. Additionally, Antiproliferative agent-64 suppresses the proliferation of MDA-MB-231 cells with an EC50 of 7 nM.

Antiproliferative agent-66 (Compound B3) is an antiproliferative compound that induces apoptosis and causes cell cycle arrest. It demonstrates IC50 values ranging from 2.03 to 3.6 µM against SH-SY5Y neuroblastoma, HT-29 colorectal adenocarcinoma, and fibroblasts. Additionally, Antiproliferative agent-66 functions as a microtubule polymerization inhibitor with an IC50 of 0.79 µM.

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