2,4-Diamino-9H-pyrimido[4,5-b]indol-5-ols: synthesis, in vitro cytotoxic activity, and QSAR investigations |
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| Authors: | Dotzauer Bernd Grünert Renate Bednarski Patrick J Lanig Harald Landwehr Jens Troschütz Reinhard |
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| Institution: | 1. College of Chemistry, Key Laboratory of Green Chemistry and Technology in Ministry of Education, Sichuan University, Chengdu 610064, PR China;2. College of Chemistry and Biology Science, Chengdu Normal University, Haike Road Eastern Section No. 99, Chengdu Wenjiang 611130, PR China;3. State Key Laboratory of Biotherapy, Sichuan University, Chengdu 610041, PR China;4. Bioinformatics and Drug Design Group, Department of Pharmacy, National University of Singapore, Blk S16, Level 8, 3 Science Drive 2, Singapore 117543, Singapore;1. Università degli Studi di Milano – Department of Chemistry; INSTM Milano Unit, Via Golgi 19, 20133 Milano, Italy;2. C.N.R. – I.S.T.M., Via Golgi 19, 20133 Milano, Italy;3. Università di Pavia, Dipartimento di Chimica, Via Taramelli 16, 27100 Pavia, Italy;4. Ecole Polytechnique Fédérale de Lausanne, Institut des sciences et ingénierie chimiques, EPFL SB ISIC GGEC, CH J2 489 (Bât. CH) Station 6, CH-1015 Lausanne, Switzerland |
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| Abstract: | A series of novel 2,4-diaminopyrimido4,5-b]indol-6-ols has been synthesized and the in vitro cytotoxic activities were evaluated against four human cancer cell lines originating from solid tumors. An increase in activity was observed when a heteroaromatic ring was annulated on side g of the pyrimido4,5-b]indole system to give compounds with activities comparable to ellipticine and cisplatin. To understand the experimental cytotoxic activities, QSAR investigations were performed, which showed a very good linearity between the experimental and predicted IC(50). |
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