Development of novel naphthalimide derivatives and their evaluation as potential melanoma therapeutics

Ugir Hossain Sk, A. S. Prakasha Gowda, Melissa A. Crampsie, Jong K. Yun, Thomas E. Spratt, Shantu Amin, Arun K. Sharma

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

Abstract

Synthesis and anti-melanoma activity of various naphthalimide analogs, rationally modified by introducing isothiocyanate (ITC) and thiourea (TU) functionalities, found in well-known anti-cancer agents, is described. The structure-activity relationship comparison of the novel agents in inhibiting cancer cell growth was evaluated in various melanoma cell lines. Both ITC and TU analogs effectively inhibited cell viability and induced apoptosis in various human melanoma cells. Nitro substitution and increase in alkyl chain length, in general, enhanced the apoptotic activity of ITC derivatives. All the new compounds were well tolerated when injected intraperitoneal (i.p.) in mice at effective doses at which both the ITC and TU derivatives inhibited melanoma tumor growth in mice following i.p. xenograft. The nitro substituted naphthalimide-ITC derivative 3d was found to be the most effective in inducing apoptosis, and in inhibiting melanoma cell and tumor growth.

Original languageEnglish (US)
Pages (from-to)3331-3338
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number8
DOIs
StatePublished - Aug 1 2011

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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