Screen Reader Access   

People : Scientific : Faculty & Scientists

DR. DINESH MAHAJAN, Ph.D. 

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.

Publications in 2018:

  • Electrophilic activation of carboxylic anhydrides for nucleophilic acylation reactionsVarun Kumar, Anil Rana, Chhuttan Lal Meena, Nidhi Sharma, Yashwant Kumara & Dinesh Mahajan* Synthesis 2018; Accepted. (IF 2.7);  https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0037-1609564
  • A practically simple, catalyst free and scalable synthesis of N-substituted ureas in water; Lata Tiwari, Varun Kumar, Bhuvesh Kumar and Dinesh Mahajan*;  RSC ADV 8 (38), 21585-21595. (IF 3.1); https://pubs.rsc.org/en/content/articlehtml/2018/ra/c8ra03761b
  • Triflic anhydride promoted synthesis of primary amides and their conversion to nitriles; Anil Rana, Varun Kumar, Lata Tiwari, Anamika Thakur, Chhuttan Lal Meena, Dinesh Mahajan* SynOpen 2 (02), 0180-01912018; https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0037-1610154
  • Spermine detection from urine and blood serum using ionic self-assembly of benzimidazolium based dipod and dodecylsulfate; Neetu Tripathia, Prabhpreet Singha, Vijay Luxamib, Dinesh Mahajan, Subodh Kumar Sensors and Actuators B: Chemical 2018, 552-561.(IF 5.1); https://www.sciencedirect.com/science/article/pii/S0925400518309523
  • Acetylenic Ester Promoted Tandem Ring Opening and Cyclizations of Dienyl Thiazolidin-4-ones: A Facile and Chemoselective Synthesis of Functionalized Pyridine-2-Carboxylates Bilash Kuila, Dinesh Mahajan, Kapil Kumar, Prabhpreet Singh, Gaurav Bhargava; Synlett 2018; 29(04): 509-512. (IF 2.3)

Publications before 2018:

  • 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)

Inventor in more than 23 filed patent applications in last seven years i.e. 2011-2018. Out of these, 14 are published and available online as PCT applications. 9 are granted in US, Japan, Europe and China.

  1. Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion, WO/2014/115167; PCT/IN2014/000048; National Phase: China, US, EU and JP.
  2. Novel triazine compounds for Pi3K/mTOR pathway, WO2014016849; PCT/IN2013/000458;CN104582707A, EP2874632A2, EP2874632A4, US20150197515
  3. Novel triazine compounds, PCTIN2012000055 Grant Number: 09481670
  4. 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), PCTIN2012000248; Grant Number: 09359376 Grant Date: 07.06.2016
  5. Novel compounds, their preparation and their uses, US2013063560 (A new technology patent to address low solubility and bioequivalence of APIs and NCEs).
  6. Methods of treating tumoral diseases, or bacterial or viral infections, PCT US20170000789; US 15266802
  7. A novel process for synthesis of polyphenols (A process patent for non-infringing route of chiral natural product),  PCT/IN2012/000052; CN103582635A, EP2668176A2, EP2668176A4, US9428482,
  8. Novel approach for synthesis of catechins (A process patent for non infringing route for a chiral natural product),  PCT/IN2014/000061; CN105026384A, EP2948437A2, EP2948437A4, US9556140, US20150368223
  9. Flavonoid compounds, PCT/US2012/049767;CN103987704A,EP2739613A4,US9187448, US20140256741
  10. Novel compounds, their synthesis and their uses, US09487500
  11. Novel compounds and anti-tubercular agents, PCT/IN2015/000226 National Phase: China, US, EU and JP.
  12. Novel compounds and inhibition of AKT kinase, IN2014DEL237 20140128 
  13. Novel analogues of epicatechin and related polyphenols, PCT/IN2014/000213; CN105283179A, EP2981260A2, EP2981260A4, US20160039781
  1. Development and PoC validation of a novel approach to treat HIV infection by integrating anti-viral activity with stimulation of host cell innate immunity started from 25th May 2017 for two years From DBT- under CRS scheme  from BIRAC-BT/CRS0200/CRS -10/16.
  2. Chemical investigation and therapeutic evaluation for linking marker compound(s) with anti-diabetic potential of young shoots of Wendlandia glabrata D.C. and fruits of Phoebe cooperiana, used by indigenous ST people of Arunachal Pradesh From DBT Sanction Order No. BT/PR24712/NER/95/828/2017 dated June 4, 2018.

 


MS. NIDHI SHARMA
TECHNICAL ASSISTANT

MR. GANESH PRASAD
LAB ASSISTANT

MS. LATA TIWARI
JUNIOR RESEARCH FELLOW

MR. NAVEEN KUMAR
LAB TECHNICIAN

DR. ARUN KUMAR
RESEARCH ASSOCIATE-I