Nazish Siddiqui

Synthesis and anti-tumor evaluation of B-ring substituted steroidal pyrazoline derivatives

The synthesis and anti-tumor activity screening of new steroidal derivatives (4-18) containing pharmacologically attractive pyrazoline moieties are performed. During in vitro anticancer evaluation, the newly synthesized compounds displayed moderate to good cytotoxicity on cervical and leukemia cancer cell lines. In addition these compounds were found to be nontoxic to normal cell (PBMCs) (IC50>50 μM). The structure-activity relationship is also discussed. The most effective anticancer compound 9 was found to be active with IC50 value of 10.6 μM. It demonstrated significant antiproliferative influence on Jurkat cell lines. The morphological changes and growth characteristics of HeLa cells treated with compound 4 were analyzed by means of SEM.

Spectrophotometric determination of the total phenolic content, spectral and fluorescence study of the herbal Unani drug Gul-e-Zoofa (Nepeta bracteata Benth)

Objectives This study quantitatively determined the total phenolic contents in ethanolic and aqueous extracts of Gul-e-Zoofa (flowers of Nepeta bracteata Benth) using a spectrophotometric method. We also performed a spectral study (UV and IR) of the ethanolic extract and a fluorescence study of the powdered drug and successive extracts to identify and characterize the genuine herbal drug, which has not been previously performed. Methods The total phenolic content was determined quantitatively using the Folin Ciocalteu reagent, with Gallic acid as the standard. The fluorescence characteristics of the powdered drug and successive extracts with and without chemical treatment during the day and under a UV light were recorded. The UV and IR spectra of the alcoholic extract of Gul-e-Zoofa were recorded using a spectrometer. Results The total phenolic contents of the alcoholic and aqueous extracts were found to be 326.28 and 319.14 mg/g of the Gallic acid equivalent (GAE), respectively. The wavelength of the maximum absorption in the UV spectrum was 320 nm, and the characteristic frequencies in the IR spectrum were 3465.31, 3220.07, 2927.3, 2856.1, 1709.07, 1610.19, 1404.5, 1250.2, 1056.42, 823.04, 775.58, 577.81, and 463.10 cm−1. The fluorescence characteristics of the powdered drug were also observed. Conclusion This spectral and fluorescence study of the drug will be helpful for confirming the identity and purity of the genuine drug. The total phenolic content will be helpful for developing new drugs and standardizing the drug. The presence of a high total phenolic content shows that the flowers of N. bracteata Benth may possess antioxidant properties, which could lead to a new field of research in the future.

SINGLE-STEP SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL STUDIES OF NOVEL STEROIDAL 1', 2', 3'- THIADIAZOLES

ABSTRACT A convenient one-step synthesis of steroidal thiadiazoles 7-9 from steroidal 6-ketone semicarbazones 1-3 with thionyl chloride has been reported. The steroidal 6-ketone thiosemicarbazones 4-6 under similar reaction conditions also provided the same products 7-9 . The structures of these newly synthesized compounds have been established on the basis of their IR, 1 H NMR and 13 C NMR, elemental and analytical data. The synthesized compounds were screened for in vitro antimicrobial activity against different bacterial (gram positive and gram negative) and fungal strains. All the synthesized compounds showed significant activity against various micro-organisms. Keywords: Steroidal thiadiazoles, Semicarbazones, thiosemicarbazones, Thionyl chloride, Antimicrobial activity. e-mail: nazish_sadat@rediffmail.com INTRODUCTION Recent studies reveals that incorporation of hetero atom (N/O/S) enhances the biological activities of steroidal molecules. The importance of heterocyclic compounds has long been recognized in the field of synthetic organic chemistry and thiadiazoles are well documented, especially after the discovery that some thiadiazoles are associated with wide variety of physiological activities such as antiaflatoxigenic