Synthesis and antiproliferative activities of indolin-2-one derivatives bearing amino acid moieties.

نویسندگان

  • Mathieu Sassatelli
  • Eric Debiton
  • Bettina Aboab
  • Michelle Prudhomme
  • Pascale Moreau
چکیده

A convenient synthesis of indolin-2-ones substituted in the 3 position by an aminomethylene group bearing different amino acid moieties is described. Their antiproliferative activities were evaluated toward a panel of human solid tumor cell lines (PC 3, DLD-1, MCF-7, M4 Beu, A549, PA 1) and healthy cell lines (a murine fibroblast L929 and a human fibroblast primary culture).

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and biological evaluation of 3-substituted-indolin-2-one derivatives containing chloropyrrole moieties.

Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4' position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as ...

متن کامل

One-pot synthesis of tetrahydropyrimido[4,5-b]quinoline derivatives using sulfonic acid functionalized SBA-15 and their antimicrobial activities

A Simple and efficient method for synthesis of tetrahydropyrimido[4,5-b]quinoline derivatives via three component reaction of aromatic aldehydes, dimedone and 6-amino uracil derivatives using a catalytic amount of sulfonic acid functionalized nanoporous silica (SBA-15-Pr-SO3H) is described. The advantages of this method are easy and clean work-up, high yield, mild reaction c...

متن کامل

Synthesis and biological evaluation of diversely substituted indolin-2-ones.

The synthesis of indolin-2-one derivatives substituted in the 3-position by an aminomethylene group bearing either an ornithine or a lysine residue is described. The inhibitory activities of these compounds toward a panel of eight kinases were examined. Furthermore, the antibacterial activities of the prepared compounds were tested against two Gram-positive bacteria Bacillus cereus and Streptom...

متن کامل

One-pot synthesis of tetrahydropyrimido[4,5-b]quinoline derivatives using sulfonic acid functionalized SBA-15 and their antimicrobial activities

A Simple and efficient method for synthesis of tetrahydropyrimido[4,5-b]quinoline derivatives via three component reaction of aromatic aldehydes, dimedone and 6-amino uracil derivatives using a catalytic amount of sulfonic acid functionalized nanoporous silica (SBA-15-Pr-SO3H) is described. The advantages of this method are easy and clean work-up, high yield, mild reaction c...

متن کامل

Tetramethylguanidiniumtriflate catalyzed Henry reaction of isatins: An efficient synthesis of 3-hydroxy-3-(nitromethyl)indolin-2-one derivatives and their anti-diabetic activity

The ionic liquid, N,N,N,N-tetramethylguanidiniumtriflate (TMGTf) was found to be an efficient catalyst solvent for Henry reaction between nitromethane and isatin derivatives to provide 3-hydroxy-3-(nitromethyl)indolin-2-one under mild conditions. The ionic liquid amenable to successive recycling without appreciable decrease in activity. Synthesized compounds have been screened for their anti-di...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:
  • European journal of medicinal chemistry

دوره 41 6  شماره 

صفحات  -

تاریخ انتشار 2006