A safe and efficacious Pt(II) anticancer prodrug: design, synthesis, in vitro efficacy, the role of carrier ligands and in vivo tumour growth inhibition

Pradip Kumar Dutta; Rupali Sharma; Smita Kumari; Ravindra Dhar Dubey; Sujit Sarkar; Justin Paulraj; Gonela Vijaykumar; Manoj Pandey; L. Sravanti; Mallik Samarla; Hari Sankar Das; Yashpal; Heeralal B.; Ravinder Goyal; Nimish Gupta; Swadhin K. Mandal; Aniruddha Sengupta; Arindam Sarkar

doi:10.1039/C8CC06586A

A safe and efficacious Pt(ii) anticancer prodrug: design, synthesis, in vitro efficacy, the role of carrier ligands and in vivo tumour growth inhibition†

Pradip Kumar Dutta,‡^a Rupali Sharma,‡^a Smita Kumari,‡^a Ravindra Dhar Dubey,^a Sujit Sarkar,^a Justin Paulraj,^a Gonela Vijaykumar,

^b Manoj Pandey,^a L. Sravanti,§^c Mallik Samarla,^a Hari Sankar Das,^b Yashpal,^a Heeralal B.,^a Ravinder Goyal,^a Nimish Gupta,

^ac Swadhin K. Mandal,

^b Aniruddha Sengupta*^ac and Arindam Sarkar

*^ac

Author affiliations

* Corresponding authors

^a Invictus Oncology Pvt. Ltd., 465 Patparganj Industrial Area, Delhi 110092, India
E-mail: asarkar@indiainnovationcenter.org, asengupta@indiainnovationcenter.org

^b Department of Chemical Sciences, Indian Institute of Science Education and Research-Kolkata, Mohanpur – 741252, India

^c India Innovation Research Center, 465 Patparganj Industrial Area, Delhi 110092, India

Abstract

Diaminocyclohexane-Pt(II)-phenalenyl complexes (1 and 2) showed an appropriate balance between efficacy and toxicity. Compound 2 showed nearly two-fold higher tumour growth inhibition than oxaliplatin in a murine NSCLC tumour model, when a combined drug development approach was used. The fluorescent properties of phenalenone were utilized to understand the mechanistic details of the drug.

Chemical Communications

A safe and efficacious Pt(ii) anticancer prodrug: design, synthesis, in vitro efficacy, the role of carrier ligands and in vivo tumour growth inhibition†

Abstract

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A safe and efficacious Pt(II) anticancer prodrug: design, synthesis, in vitro efficacy, the role of carrier ligands and in vivo tumour growth inhibition

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