Metal‐(Acyclic Diaminocarbene) Complexes Demonstrate Nanomolar Antiproliferative Activity against Triple‐Negative Breast Cancer

Author:

Katkova Svetlana A.1ORCID,Bunev Alexander S.2ORCID,Gasanov Rovshan E.2ORCID,Khochenkov Dmitry A.23ORCID,Kulsha Andrey V.4ORCID,Ivashkevich Oleg A.5ORCID,Serebryanskaya Tatiyana V.5ORCID,Kinzhalov Mikhail A.1ORCID

Affiliation:

1. Saint Petersburg State University 7/9 Universitetskaya Nab. St. Petersburg 199034 Russian Federation

2. Medicinal Chemistry Center Togliatti State University Belorusskaya 14 Togliatti 445020 Russian Federation

3. Blokhin National Medical Research Center of Oncology Kashirskoe Shosse 24 115478 Moscow Russian Federation

4. Department of Chemistry Belarusian State University Leningradskaya 14 220006 Minsk Belarus

5. Research Institute for Physical Chemical Problems Belarusian State University Leningradskaya 14 220006 Minsk Belarus

Abstract

AbstractHydrolytically stable PdII and PtII complexes supported by acyclic diaminocarbene ligands represent a novel class of structural organometallic anticancer agents exhibiting nanomolar antiproliferative activity in a panel of cancer cell lines (IC50 0.07–0.81 μM) and up to 300‐fold selectivity for cancer cells over normal primary fibroblasts. The lead drug candidate was 300 times more potent than cisplatin in vitro and showed higher efficacy in reducing the growth of aggressive MDA‐MB‐231 xenograft tumors in mice.

Funder

Russian Science Foundation

Publisher

Wiley

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