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Scientist E
+91-129-2876476  (+91-129-2876476)
dinesh.mahajan [at] thsti [dot] res [dot] in
Ph.D. in Synthetic Organic Chemistry

Dr. Dinesh is an experienced medicinal chemist and a drug discovery scientist. He has around 15 year of medicinal chemistry experience in academic and industrial setups. Dinesh obtained his Master and PhD in synthetic organic chemistry with emphasis on designing, synthesis and synthetic evaluation of chiral organocatalysts to mimic enzymes for asymmetric synthesis in water. His PhD research work was published in leading journals of organic chemistry and is recognized with high citations. This was followed by a short stay at New Drug Discovery Research (NDDR), Ranbaxy INDIA as a medicinal chemist. While working for Ranbaxy, he got exposed to parallel and library synthesis using combinatorial approach. Dr Dinesh spend two years as a postdoctoral fellow (Dec 2006 - Dec 2008) at University de Strasbourg, France formerly known as Louise Pastuer University. There he worked on the designing and synthesis of cytochrome C oxidase model based on porphyrin core. This involves multistep synthesis of porphyrin based biomimics of Cyt C Oxidase. In late 2008, Dinesh joined a biotechnology based start-up company “Sphaera Pharma” In INDIA as a founder member of drug discovery team. At Sphaera, he led the efforts of establishing a medicinal chemistry laboratory, analytical chemistry lab and a team of dedicated medicinal chemistry scientists starting from scratch. At Sphaera, as drug discovery team leader, his major focus revolves around pre-clinical drug discovery that involves hit identification to lead optimization leading to IND candidate identifications followed by process R&D of leads and their cGMP manufacturing. The pre-clinical discovery efforts involves generation of SAR understanding around identified hit or lead, optimization of identified lead for ADMET properties based on screening across various in vitro and in vivo pharmacology assays and process R&D of the identified lead to support in vivo studies as well as cGMP manufacturing. During his stay at Sphaera Pharma, he got a good hand on experience in designing in vitro and in vivo pharmacology assays while his interactions with pre-clinical pharmacology team along with CMC and cGMP manufacturing. His drug discovery experience spans around different therapeutic areas e.g. oncology, metabolic disorder, host based approach for infectious diseases. He has a successful experience of pushing discovery project from conception of idea to IND candidate discovery in oncology, infectious disease and metabolic disorders. Notably, two of the identified leads by his efforts are under phase 2 clinical development, other two leads are under IND enabling studies and few more are in late stage pre-clinical development. He is inventor in more than 16 patent applications in different therapeutic domains. He is also a key inventor in developing a chemical transformation based drug modification technology, which aids drug development of lead molecules or approved APIs by increasing solubility and altering their pharmacokinetic profiles. His efforts as leader of drug discovery group resulted in identification and development two technologies to aid drug discovery and development. Two of the technologies and 2 IND candidates developed are out-licensed in US which progressed to clinical development. Presently, he is working at DDRC as scientist E and leading medicinal chemistry efforts to support translational research leading to identification and development of lead molecules and new targets for drug discovery.

  • Killing Glioma 'Stem-like' Cells via Drug-Induced Relocation of Endosomal Urokinase Proteins Fredric A Gorin, Nagarekha Pasupuleti, Dinesh Mahajan, Sundeep Dugar; Jun 2016 · Anti-cancer agents in medicinal chemistry. (IF 2.8)
  • A Facile and Chemoselective Synthesis of 1,4-Benzodiazepin-2-ones and Dienyl Thiazolidin-4-onesBilash Kuila, Yogesh Kumar, DineshMahajan, Prabhpreet Singh, Pankaj, Gaurav Bhargava;  RSC Adv., 2016,6, 57485-57489.(IF 3.3).
  • Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines Sundeep Dugar, Frank P. Hollinger, Dinesh Mahajan*, Somdutta Sen, Bilash Kuila, Reena Arora, Yogesh Pawar, Vaibhav Shinde Mahesh Rahinj, Kamal K. Kapoor, Rahul Bhumkar, Santosh Rai, and Rakesh KulkarniACS Med. Chem. Letters 2015 ASAP DOI: 10.1021/acsmedchemlett.5b00322; (IF 3.2).
  • New small molecules that kill hypoxically transformed glioma stem-like cells Nagarekha Pasupuleti*, Anthony Valenzuela, Yamini Manohar, Dinesh Mahajan, Sundeep Dugar, Jann Sarkaria, Fredric Gorin,  Neuro-Ooncology 17(SUPPL 5):V31-V31 · NOVEMBER 201. (IF 5.56)
  • Preclinical activity of dual PI3K/mTOR inhibitor SPR965 in multiple myeloma Jeremy T. Larsen, Vijay Ramakrishnan, Jessica Haug, Teresa Kimlinger, Somdutta Sen, Dinesh Mahajan, Sundeep Dugar, S. Vincent Rajkumar, Shaji K. Kumar Cancer Research 75(15 Supplement):2653-2653 August 2015; doi: 10.1158/1538-7445.AM2015-2653. (IF 9.33)
  • SPR965: an oral PI3K/ mTOR C1/C2 inhibitor for the treatment of solid tumors Arora,R.; Dutta, B. K.; Goel, R.; Hollinger, F. P.; Kuila, B.; Mahajan, D.; Mahapatra, A. R.; Sagar, M.; Sen, S.; Sharma, A.;  Dugar, S Cancer Res October 1, 2014 74; 4515;doi: 10.1158/1538-7445.AM2014-4515; (IF 9.33)
  • Synthesis and evaluation of pyrrolotriazine based novel small molecules as selective inhibitors for PI3K kinase Sundeep Dugar, Frank Hollinger, Somdutta Sen, Bilash Kuila and Dinesh Mahajan*Bio. Org. Med Chem Letters 2015, 15, 3142. (IF 2.4)
  • A concise and efficient synthetic approach to substituted morpholines. Sundeep Dugar, Amit Sharma, Bilash Kuila and Dinesh Mahajan*, Synthesis 2015, 47, 712-720. (IF 2.7)
  • Nickel catalyzed [3+2] cycloaddition reaction of bis(methylenecyclopropane) with cyclic and acyclic dienophilesBilash Kuila, DineshMahajan, Prabhpreet Singh, Gaurav Bhargava Tetrahedron Letters2015, 56, 1307-1311.(IF 2.4.
  • Metal-free diastereoselective synthesis of diaza-bicyclo[3.2.0]heptan-7-one and its transformation to functionalized proline esters.Yogesh Kumar, Bilash Kuila, DineshMahajan, Prabhpreet Singh, Balaram Mohapatra, Gaurav BhargavaTetrahedron Letters2014, 2793-2795. (IF 2.4)
  • Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion India WO2014IN00048 20140123Filed January 23, 2013
  • Novel Triazine Compounds for Pi3K/mTOR Pathway United States WO2013IN00458 20130723 Filed August 23, 2012 Also Published as WO2014016849 (A9) WO2014016849 (A3)
  • Novel Triazine Compounds United States US2013303516 (A1) Filed January 25, 2011 Also published as WO2012101654 (A2) WO2012101654 (A3)
  • Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds (A new technology patent to address low solubility and bioequivalence of APIs and NCEs) United States US201214110373 20120409 Filed April 8, 2011
  • Also Published as WO2012137225 (A1) JP2014514300 (A) EP2693876 (A1) CN103607888 (A)
  • Novel compounds, their preparation and their uses United States WO2013US63560 20131004 Filed October 4, 2013 Also Published as US2014100225 (A1)
  • A novel process for synthesis of polyphenols (A process patent for non infringing route of chiral natural product) United States PCT/IN2012/000052 Filed January 24, 2012 Also Published as WO2012101652 (A2) WO2012101652 (A3) US2014031421 (A1) TW201309662 (A) JP2014509312 (A) EP2668176 (A2)
  • Novel approach for synthesis of catechins (A process patent for non-infringing route for a chiral natural product) India WO2014IN00061 20140127 Filed January 26, 2013
  • Flavonoid compounds United States PCT/US2012/049767 Filed August 6, 2012
  • Novel compounds, their synthesis and their uses  United States Patent Application WO2013IN00607 20131007
  • Novel compounds and anti-tubercular agents WO2015IN00226 20150601
  • Novel compounds and inhibition of AKT kinase IN2014DEL237 20140128 
  • Novel analogues of epicatechin and related polyphenols  European Patent Application WO2014162320

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