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Structure-activity relationships of new Organotin(IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7 and HeLa human cancer cell lines

Ullah, Hussain ; Previtali, Viola ; Mihigo, Helene B. ; Twamley, Brendan ; Rauf, Muhammad Khawar ; Javed, Fatima ; Waseem, Amir ; Baker, Robert J. ; Rozas, Isabel

European journal of medicinal chemistry, 2019-11, Vol.181, p.111544-111544, Article 111544 [Periódico revisado por pares]

France: Elsevier Masson SAS

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Título:
Structure-activity relationships of new Organotin(IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7 and HeLa human cancer cell lines
Autor: Ullah, Hussain ; Previtali, Viola ; Mihigo, Helene B. ; Twamley, Brendan ; Rauf, Muhammad Khawar ; Javed, Fatima ; Waseem, Amir ; Baker, Robert J. ; Rozas, Isabel
Assuntos: Anticancer agents ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Apoptosis ; Cell growth inhibition ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; HeLa ; HeLa Cells ; HL-60 ; HL-60 Cells ; Humans ; MCF-7 ; MCF-7 Cells ; Molecular Structure ; Organotin Compounds - chemical synthesis ; Organotin Compounds - chemistry ; Organotin Compounds - pharmacology ; Organotin(IV)complexes ; Structure-Activity Relationship ; Structure-activity relationships
É parte de: European journal of medicinal chemistry, 2019-11, Vol.181, p.111544-111544, Article 111544
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SourceType-Scholarly Journals-1
ObjectType-Feature-2
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Descrição: There is a growing interest in the cancer cell growth inhibitory effects of organotin (IV) compounds and, accordingly, a new series of dimethyl-, di-(n-butyl)-, diphenyl- and chloro-phenyl tin(IV) complexes with a Schiff base core were prepared. Their binding to DNA was assessed by UV thermal denaturation showing no interaction and by UV–vis titration exhibiting moderate interaction by intercalation. Complexes having n-butyl substituents were more potent and cytotoxic against human leukemia, breast and cervical cancer cell lines than other organotin(IV) complexes tested. Unfortunately, some of these compounds showed similar cytotoxicity in a non-cancerous cell line. We may conclude that cytotoxic activity was dependent on the nature (lipophilicity and size, according to the structure-activity relationship studies) and substitution pattern on the different structures. These results may aid in the rational design of metallodrugs, expanding the scope of organotin complexes in formulating new metal based drugs with dibutyl moieties. [Display omitted] •Organotin(IV) complexes have been prepared with diverse lipophilic substituents.•Five of these complexes' X-ray structures were solved confirming their coordination.•Bis-(2-hydroxybenzylidene)malonohydrazone Sn(IV) complex do not bind to DNA.•Di-(n-butyl) complexes show good cytotoxicity in HL-60, MCF-7 and HeLa cancer cells.•Bis-(2-hydroxybenzylidene)malonohydrazone Sn(IV) complex strongly induces apoptosis.
Editor: France: Elsevier Masson SAS
Idioma: Inglês

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Structure-activity relationships of new Organotin(IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7 and HeLa human cancer cell lines

Ullah, Hussain ; Previtali, Viola ; Mihigo, Helene B. ; Twamley, Brendan ; Rauf, Muhammad Khawar ; Javed, Fatima ; Waseem, Amir ; Baker, Robert J. ; Rozas, Isabel

France: Elsevier Masson SAS

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