CisPlatin And Related Compounds.
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Cisplatin is a chemotherapy drug discovered in 1965 to inhibit cell division. It was found to be effective against tumors. Cisplatin is synthesized through a reaction involving Magnus's Green Salt. Carboplatin is a related compound that replaces cisplatin's chloride ligands with cyclohexane dicarboxylate ligands, giving it a longer half-life and reduced nephrotoxicity but also susceptibility to resistance. Dicycloplatin forms polymer chains through hydrogen bonding between carboplatin and cyclohexane dicarboxylate, making it more potent than carboplatin while maintaining similar myelosuppressive effects.
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![Introduction
Cisplatin, or cis- diamminedichloroplatinum (II) - a well known
chemotherapeutic drug.
In 1965, B.Rosenberg discovered electrolysis of platinum electrodes
generated a soluble platinum complex which inhibited binary fission in E.
coli bacteria.
His finding led to observation that cis-[PtCl2(NH3)2] was indeed highly
effective at regressing the mass of sarcomas (malignant tumors).](data:image/gif;base64,R0lGODlhAQABAIAAAAAAAP///yH5BAEAAAAALAAAAAABAAEAAAIBRAA7)
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Aromatase Inhibitors (AIs): These drugs, including anastrozole, letrozole, and exemestane, lower estrogen levels by inhibiting the aromatase enzyme, which converts androgens to estrogen in peripheral tissues. AIs are generally preferred in postmenopausal women due to their efficacy and safety profile compared to tamoxifen.
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Endocrine Therapy with mTOR Inhibitors: Everolimus, an mTOR inhibitor, can be added to endocrine therapy for patients who have developed resistance to aromatase inhibitors.
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CisPlatin And Related Compounds.
- 1. Synthesis, Mechanism and Medicinal applications of cis- platin and related compounds By- Pratik Kharat MSc Chemistry Part I Ramnarain Ruia College
- 2. Introduction Cisplatin, or cis- diamminedichloroplatinum (II) - a well known chemotherapeutic drug. In 1965, B.Rosenberg discovered electrolysis of platinum electrodes generated a soluble platinum complex which inhibited binary fission in E. coli bacteria. His finding led to observation that cis-[PtCl2(NH3)2] was indeed highly effective at regressing the mass of sarcomas (malignant tumors).
- 5. Other cisplatin related complexes Carboplatin It has a bidentate dicarboxylate (the ligand is CycloButane Dicarboxylic Acid, CBDCA) in place of the two chloride ligands as Leaving Group. A retention half-life of 30 hours for carboplatin, compared to 1.5-3.6 hours in the case of cisplatin. Non Nephrotoxic . Susceptible to resistance and is Myelosuppressive.
- 6. Other Cisplatin Related complexes Dicycloplatin O-H...O bond between the hydroxyl group of CBDC with carboxyl oxygen atom. Creates one- dimensional polymer chain of carboplatin and CBDC. The second one is N-H...O bond between the ammonia group of carboplatin and oxygen of CBDC creates the two-dimensional polymer chain of carboplatin and CBDC. Myelosuppressive Potency is similar to carboplatin but it is much effective in action.
- 7. References Dhara SC (1970). "Cisplatin". Indian J. Chem. 8: 123–134. Alderden RA, Hall MD, Hambley TW (2006). "The Discovery and Development of Cisplatin". J. Chem. Educ. 83 (5): 728. Bibcode:2006JChEd..83..728A. doi:10.1021/ed083p728. S2CID 29546931. https://www.sciencedirect.com/topics/chemistry/carboplatin >Review • Braz. J. Pharm. Sci. 50 (4) • Oct-Dec 2014 • https://doi.org/10.1590/S1984-82502014000400004 >Effect of Dicycloplatin, a Novel Platinum Chemotherapeutical Drug, on Inhibiting Cell Growth and Inducing Cell Apoptosis (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3495782/)