Related Products of 43142-76-3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Ethyl 5-chloro-3-formyl-1H-indole-2-carboxylate, is researched, Molecular C12H10ClNO3, CAS is 43142-76-3, about Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic antiproliferative activity. Author is Mohamed, Fatma A. M.; Gomaa, Hesham A. M.; Hendawy, O. M.; Ali, Asmaa T.; Farghaly, Hatem S.; Gouda, Ahmed M.; Abdelazeem, Ahmed H.; Abdelrahman, Mostafa H.; Trembleau, Laurent; Youssif, Bahaa G. M..
New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide derivatives I (R1, R2 = H, Me; R3 = Me2N, pyrrolidin-1-yl, piperidin-1-yl, etc., R4 = H; R3 = H, R4 = pyrrolidin-1-yl, morpholin-4-yl, etc.) and II [R5 = 1-benzylpiperidin-3-yl, 1-benzylpyrrolidin-3-yl, 2-(morpholin-4-yl)ethyl] has been designed, synthesized, and tested for antiproliferative activity against a panel of cancer cell lines. The results showed that p-substituted phenethyl derivatives showed superior antiproliferative activity compared to their m-substituted counterparts. Compounds I (R1 = R2 = R4 = H; R3 = piperidin-1-yl, morpholin-4-yl) and I (R1 = R2 = R3 = H; R4 = piperidin-1-yl, morpholin-4-yl) displayed promising EGFR inhibitory activity as well as an increase in caspase 3 levels. Compounds I (R1 = R2 = R4 = H; R3 = piperidin-1-yl, 4-morpholin-4-yl) increased caspase-8 and 9 levels, as well as inducing Bax and decreasing Bcl-2 protein levels. The compound I (R1 = R2 = R4 = H; R3 = morpholin-4-yl) demonstrated cell cycle arrest at pre-G1 and G2/M phases. The results of the docking study into the active site of EGFR revealed strong fitting of the new compounds with higher binding affinities compared to erlotinib.
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