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  • Title: Synthesis and biological evaluation of new [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines against Leishmania donovani.
    Author: Gupta L, Sunduru N, Verma A, Srivastava S, Gupta S, Goyal N, Chauhan PM.
    Journal: Eur J Med Chem; 2010 Jun; 45(6):2359-65. PubMed ID: 20371140.
    Abstract:
    A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01-57.78 microM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I.=56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.
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