@article {46995,
	title = {Highly enantioselective synthesis of sitagliptin},
	journal = {Asian Journal of Organic Chemistry},
	volume = {9},
	year = {2020},
	month = {FEB},
	pages = {189-191},
	type = {Article},
	abstract = {<p>A highly enantioselective synthesis of sitagliptin, a potent DPP-4 inhibitor, is reported. Explicitly identified chiral FerroLANE ligands in the presence of rhodium catalyze the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98\% ee). The process was scaled up to 5 g and the final product was isolated as a phosphate salt with \&gt;99\% ee.</p>
},
	keywords = {asymmetric hydrogenation, catalysis, FerroLANE ligands, Rhodium, sitagliptin},
	issn = {2193-5807},
	doi = {10.1002/ajoc.201900709, Early Access Date = JAN 2020},
	author = {Khopade, V. Kishor and Sen, Anirban and Birajdar, Rajkumar S. and Paulbudhe, Uday P. and Kavale, Dattatry S. and Shinde, Prashant S. and Mhaske, Santosh B. and Chikkali, Samir H.}
}
@article {47061,
	title = {Photoactivatable prodrug for simultaneous release of mertansine and CO along with a BODIPY derivative as a luminescent marker in mitochondria: a proof of concept for NIR image-guided cancer therapy},
	journal = {Chemical Science},
	volume = {12},
	year = {2021},
	month = {FEB},
	pages = {2667-2673},
	type = {Article},
	abstract = {<p>Controlled and efficient activation is the crucial aspect of designing an effective prodrug. Herein we demonstrate a proof of concept for a light activatable prodrug with desired organelle specificity. Mertansine, a benzoansamacrolide, is an efficient microtubule-targeting compound that binds at or near the vinblastine-binding site in the mitochondrial region to induce mitotic arrest and cell death through apoptosis. Despite its efficacy even in the nanomolar level, this has failed in stage 2 of human clinical trials owing to the lack of drug specificity and the deleterious systemic toxicity. To get around this problem, a recent trend is to develop an antibody-conjugatable maytansinoid with improved tumor/organelle-specificity and lesser systematic toxicity. Endogenous CO is recognized as a regulator of cellular function and for its obligatory role in cell apoptosis. CO blocks the proliferation of cancer cells and effector T cells, and the primary target is reported to be the mitochondria. We report herein a new mitochondria-specific prodrug conjugate (Pro-DC) that undergoes a photocleavage reaction on irradiation with a 400 nm source (1.0 mW cm(-2)) to induce a simultaneous release of the therapeutic components mertansine and CO along with a BODIPY derivative (BODIPY(PPH3)(2)) as a luminescent marker in the mitochondrial matrix. The efficacy of the process is demonstrated using MCF-7 cells and could effectively be visualized by probing the intracellular luminescence of BODIPY(PPH3)(2). This provides a proof-of-concept for designing a prodrug for image-guided combination therapy for mainstream treatment of cancer.</p>
},
	issn = {2041-6520},
	doi = {10.1039/d0sc06270g},
	author = {Tiwari, Rajeshwari and Shinde, Prashant S. and Sreedharan, Sreejesh and Dey, Anik Kumar and Vallis, Katherine A. and Mhaske, Santosh B. and Pramanik, Sumit kumar and Das, Amitava}
}
