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• W2016800736 abstract "A series of new, water-soluble phenyl N-mustard-benzenealkylamide conjugates containing hydrophilic ω-dialkylaminoalkylamide or ω-cyclic aminoalkylamide moieties were synthesized via a bioisostere approach. These compounds have a broad spectrum of antitumor activity against a panel of human tumor cell lines. Of these derivatives, compound 18b effectively suppressed the growth of colon cancer (HCT-116), prostate cancer (PC3), and lung cancer (H460) xenografts. The growth of HCT-116 xenografts was almost completely suppressed when co-treated with compound 18b and 5-fluorouracil. Furthermore, compound 18b can induce DNA cross-linking and cell-cycle arrest at the G2/M phase. Early preclinical studies, including pharmacokinetics in rats, inhibition of the hERG, and 14 days of acute intravenous injection toxicity, suggest that compound 18b is a promising candidate for further preclinical studies. • A series of water-soluble phenyl N-mustard-benzenealkylamides were synthesized. • These compounds shows broad spectrum activity against a panel of tumor cell lines. • Compound 18b was found to have potent therapeutic efficacy in xenograft models. • The combination of 18b and 5-FU almost completely suppressed HCT-116 xenografts. • Current studies, suggest that 18b is a promising candidate for preclinical studies." @default.
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• W2016800736 date "2014-04-01" @default.
• W2016800736 modified "2023-09-23" @default.
• W2016800736 title "Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach" @default.
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• W2016800736 doi "https://doi.org/10.1016/j.ejmech.2014.02.018" @default.
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