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Presentation
by
Mr Abhishek Ghara
Department of Pharmaceutical Chemistry,
Acharya & B.M. Reddy College of Pharmacy,
Bangalore-107.
PRESENTATION - 2
“Synthesis of Triazenoazaindoles: A New Class of
Triazenes with Antitumor Activity”
INTRODUCTION:
Despite improvements in the treatment and prevention of cancer, the
number of new diagnoses continues to rise; this has fuelled substantial
interest in the development of new and effective chemotherapeutic
agents.
Compounds of the triazene class, such as dacarbazine, have been used
in the clinical management of many cancer types including brain,
leukemia.
A new compound class bearing a triazenoazaindole scaffold was
synthesized with the aim of identifying new antiproliferative agents.
SCHEME FOR SYNTHESIS:
ANTIPROLIFERATIVE ACTIVITY STUDIES:
•Cytotoxicity was determined by the MTT test after 72 hrs of
treatment with compounds in five human tumor cell lines: Jurkat (T-
cell leukemia); K-562 (chronic myeloid leukemia); CEM (T-cell
leukemia); Lovo (colon carcinoma), and A-431 (vulvar squamous
cell carcinoma).
•Cell survival expressed as GI50 , the concentration which induces
50% of inhibition of cell growth after 72 hrs of cell incubation in the
presence of the test compounds.
•Dacarbazine was used as reference compound because of its
structural similarity with triazenopyridopyrrolo derivatives.
RESULT AND DISCUSSION:
SYNTHESIS OF TRIAZENOAZAINDOLES

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SYNTHESIS OF TRIAZENOAZAINDOLES

  • 1. Presentation by Mr Abhishek Ghara Department of Pharmaceutical Chemistry, Acharya & B.M. Reddy College of Pharmacy, Bangalore-107. PRESENTATION - 2 “Synthesis of Triazenoazaindoles: A New Class of Triazenes with Antitumor Activity”
  • 2. INTRODUCTION: Despite improvements in the treatment and prevention of cancer, the number of new diagnoses continues to rise; this has fuelled substantial interest in the development of new and effective chemotherapeutic agents. Compounds of the triazene class, such as dacarbazine, have been used in the clinical management of many cancer types including brain, leukemia. A new compound class bearing a triazenoazaindole scaffold was synthesized with the aim of identifying new antiproliferative agents.
  • 4.
  • 5. ANTIPROLIFERATIVE ACTIVITY STUDIES: •Cytotoxicity was determined by the MTT test after 72 hrs of treatment with compounds in five human tumor cell lines: Jurkat (T- cell leukemia); K-562 (chronic myeloid leukemia); CEM (T-cell leukemia); Lovo (colon carcinoma), and A-431 (vulvar squamous cell carcinoma). •Cell survival expressed as GI50 , the concentration which induces 50% of inhibition of cell growth after 72 hrs of cell incubation in the presence of the test compounds. •Dacarbazine was used as reference compound because of its structural similarity with triazenopyridopyrrolo derivatives.