Denny, William A. published the artcilePotential antitumor agents. 59. Structure-activity relationships for 2-phenylbenzimidazole-4-carboxamides, a new class of minimal DNA-intercalating agents which may not act via topoisomerase II, Name: 6-Amino-3-bromo-2-methylbenzoic acid, the main research area is antitumor benzimidazolecarboxamide; antileukemic benzimidazolecarboxamide; neoplasm inhibitor benzimidazolecarboxamide; DNA minimal intercalating agent benzimidazolecarboxamide.
A series of ∼30 substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and evaluated for in vitro and in vivo antitumor activity. These compounds represent the logical conclusion to our search for “”minimal”” DNA-intercalating agents with the lowest possible DNA-binding constants Such “”2-1″” tricyclic chromophores, of lower aromaticity than the structurally-similar 2-phenylquinolines, have the lowest DNA binding affinity yet seen in the broad series of tricyclic carboxamide intercalating agents. Despite very low in vitro cytotoxicities, several of the compounds had moderate levels of in vivo antileukemic effects. However, the most interesting aspect of their biol. activity was the lack of cross-resistance shown to an amsacrine-resistant P388 cell line, suggesting that these compounds may not express their cytotoxicity via interaction with topoisomerase II. Thus, cyclization of RCHO (R = tolyl, anisyl, ClC6H4, etc.) with aminoanthranilic acid I gave benzimidazole II (R1 = OH) which was amidated with Me2N(CH2)2NH2 to give II [R1 = NH(CH2)2NMe2].
Journal of Medicinal Chemistry published new progress about Cyclocondensation reaction. 124341-06-6 belongs to class bromides-buliding-blocks, name is 6-Amino-3-bromo-2-methylbenzoic acid, and the molecular formula is C8H8BrNO2, Name: 6-Amino-3-bromo-2-methylbenzoic acid.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary