Achievements

Highlights of Scientific Contributions of

Prof. Atul Kumar

Drug discovery/ Medicinal Chemistry Contributions:

Working in area of Osteoporosis, Anti cancer, Anti-tuberculosis and Regenerative Medicines. I have several active compounds which are in different stages of drug development.

• Anti-osteoporosis

We have Design and synthesized a novel chemical Entities CDRI-99/373 (CENTHANK) which is an Anti-osteoporosis drug Candidate. DCGI permission has granted ( Feb 2017) and currently in Phase–I Clinical Trial is in progress.

• CSIR – Fast Track Translational (FTT project) from CDRI

CDRI website: Product Pipe Line- Candidate Drugs:. http://www.cdri.res.in/candidatedrug.aspx

Advantage over existing therapeutics :

CDRI-99/373 has one pot synthesis strategy, which makes it cost-effective and hence Compound has very good commercial potential. Product has advantage over existing clinically used drugs like Raloxifene and Bisphoaphonates in terms of its efficacy as well as toxicity.

• Anti Cancer

We have design and synthesized new chemical entity CDRI-S-007-1235 showing promising anticancer activity breast, colon or haematological malignancies (leukemia). Patent has been filed and Compound is in Preclinical stage and detail toxicity is in process.

CDRI website : Product Pipe Line/ Potential Leads

http://www.cdri.res.in/Potential_leads.aspx

CDRI-S-007-1235 Advantage over existing therapeutics:

• CDRI-S-007-1235 inhibits proliferation and induces apoptosis in chronic myelogenous leukemia patient (CML) samples with higher efficacy than marketed drugs Imatinib and Dasatinib.
• MND inhibits proliferation and induces apoptosis in mutant BCR-ABL harbouring patient samples (T315I) refractory to Imatinib or Dasatinib.( No TKI are active against T315I except Ponatinib ). Compound induced robust myeloid differentiation in leukemia cell-lines as well as Blast Phase and CML patients in Accelerated Phase.
• MND reduced breast, colon and leukemia cancer stem cell population and its activity was comparable to Salinomycin.

• Anti-Obesity agents:

CDRI-S-013-1593 is First in class H3R antagonist with in-vivo efficacy comparable to approved Drug Lorcaserine.

For details please see

CDRI website : Product Pipe Line/ Potential Leads http://www.cdri.res.in/S013-1593.aspx

• Anti-Tuberculosis :

Recently in Indo-French project we got a very interesting generation zero Dendrimers 16/CEF/280/281 having promising Anti-tuberculosis activity and we are going to file joint patent

• Green Chemistry:

Developed an Efficient atom and step economic (EASE) synthesis of the “smart drug” Modafinil

· Developed green synthesis of anti-tubercular natural products Tryptanthrin

· Introduced a new strategy for organic synthesis utilizing Functional Ionic Liquid and named as Functional Ionic Liquid Mediated Synthesis (FILMS) Green Chemistry 2011, 13, 2459.

· Development of First Single Nucleotide catlysed organic reaction: “Single Nucleotide Catalysed Biomimetic reductive Amination reaction Advanced Synthesis and Catalyst 352 (13): 2227–2232

· We have developed new metal Free synthetic strategy for sp3C-H activation using Iodine as catalyst for the synthesis of Azarene pyridinium Zwitterions Organic Letters 2011,13,6366.

· Developed methodology for Artemether and arteether (Antimalarial Drug) and new approach for key intermediated of Drugs Imatinib, Nilotinib (anticancer Drugs) and Oxacarbazpine (antiepileptic drug)

· First in situ generated NHC (betaine intermediate) mediated annulations reaction.