A series of novel N,N-disubstituted Et P-[2-(1H-indol-3-yl)acetyl]phosphoramidates were synthesized.All title compounds were characterized by IR, NMR (¹H, ¹³C, ³¹P) spectra, mass spectra, and C, H, N anal.The anticancer activity of the title compounds was evaluated in two human cell lines MCF-7 (breast cancer) and HeLa (Cervical cancer) cell lines by the use of the MTT assay, and the IC₅₀ values were determinedThe derivatives with substituted piperazines exhibited significant cytotoxicity against the tested cell lines at 5 μM and displayed low IC₅₀ values in the region of 5.8-8.8 μM for MCF-7 cell lines and 14.8-16.4 μM for HeLa cell lines when compared with the standard doxorubicin (5.4 and 14.2 μM).

01 Jan 2013·Chemical and Pharmaceutical BulletinQ4 · MEDICINE

Synthesis of Novel Phosphorylated Guanidine Derivatives from Cyanamide and Their Anti-inflammatory Activity

Q4 · MEDICINE

Article

Author: Kuntrapakam, Hema Kumar ; Syed, Rasheed ; Kuruva, Chandra Sekhar ; Chamarthi, Naga Raju ; Katla, Venkata Ramana

A series of novel guanidine derivatives were synthesized in three steps and their anti-inflammatory activities in vitro and in vivo evaluated. 2-Aminopyridin-3-ol (1) was reacted with thiophosphoryl chloride (2) to give a monochloride (3). It was further reacted with cyanamide to afford the corresponding cyanamine (4), which was subsequently reacted with different heterocyclic amines to form the title compounds (5a-l). The substituent in the guanidine function affected the potency of anti-inflammatory activity. The compounds having benzothiazole, fluorophenyl, and piperazinyl moieties enhanced the anti-inflammatory activity.

31 Jan 2012·ISRN Toxicology

Evaluation of Eye Irritation Potential of Aqueous Leaf Extract of Achyranthes aspera by In Vitro and In Vivo Method

Article

Author: Hema Kumar, Kuntrapakam ; Rajpal Deshmukh, Gajanan ; Venkata Satish Kumar, Chirumamilla ; Srinivasa Rao, Boddapati ; Suresh Reddy, Poojari Venkata

The present paper is an attempt to investigate the eye irritation potential of aqueous leaf extract of Achyranthes aspera by in vitro, Hen's Egg Chorioallantoic Membrane Test (HET-CAM) and in vivo acute eye irritation test in rabbits. The irritation score (IS) obtained after treatment of the extract on HET-CAM is 0.07 and that of in rabbits is 0.55, Which does not comes under either category 1 or 2 as per the harmonized integrated classification system. The aqueous extract of Achyranthes aspera showed no eye irritation properties both in vitro and in vivo methods when compared with negative control whereas positive controls showed eye irritation potential.

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