Our systematic study on 2-mercaptobenzenesulfonamide derivatives led us to discover novel anticancer,^[1–5] anti-HIV^[6,7] and antibacterial^[8] agents. Our ongoing research program aimed at the synthesis and biological evaluations of novel 2-mercaptobenzenesulfonamides (MBSA) with five-membered heterocycles located at 5 position of MBSA scaffold^[4,5] led us for finding the unconventional group of compounds bearing N-2-unsubstituted 1-benzenesulfonyl-3-hydroxyguanidine moiety, as potent in vitro cytostatic agents against numerous of NCI-60 cell lines of human leukemia, melanoma, non-small cell lung cancer, colon, CNS, renal, prostate, ovarian and breast cancers.

Nineteen of twenty four examined compounds at US, NCI (Bethesda), showed significant and broad cytostatic effect at low micromolar GI₅₀ level (mean value in the range of 1.62–18.62 µM), and mean TGI ranged from 3.72–75.86 µM, over most of 60 tested cell lines.
QSAR studies were conducted to better understand structure-activity relationship (SAR) against human cancer cells, involving CoMSIA field descriptors. Additionally, COMPARE analyses were performed for representative 11 compounds. For at least 6 compounds NCI-60 cell lines panel inhibition profiles were correlated (Pearson correlation coefficient >0.5) with dactinomycin, bruceantin, chromomycin A3 and echinomycin – nucleic acid interfering agents.

References:

1. J. Sławiński, Eur. J. Med. Chem. 39 (2004) 179–188.
2. J. Sławiński, M. Gdaniec, Eur. J. Med. Chem. 40 (2005) 377–389.
3. J. Sławiński, Z. Brzozowski, Eur. J. Med. Chem. 41 (2006) 1180–1189.
4. J. Sławiński, Z. Brzozowski, Eur. J. Med. Chem. 41 (2006) 1180–1189.
5. K. Brożewicz, J. Sławiński, Monatsh. Chem. (2012) doi: 10.1007/s00706-012-0732-6
6. C.-L. Kuo, H. Assefa, S. Kamath, Z. Brzozowski, J. Sławiński, F. Sączewski, J.K. Buolamwini, N.Neamati, J. Med. Chem. 47 (2004) 385–399.
7. Z. Brzozowski, J. Sławiński, F. Sączewski, T. Sanchez, N.Neamati, Eur. J. Med. Chem. 43 (2008) 1188–1198.
8. J. Sławiński, B. Żołnowska, D. Pirska, A. Kędzia, E. Kwapisz, J. Enzyme Inhib. Med. Chem. (2011), doi: 10.3109/14756366.2011.625024

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/25448 must be provided.