Search results for "Farmaceutica"

One pot-like regiospecific access to 1-aryl-1H-pyrazol-3(2H)-one derivatives and evaluation of the anticancer activity

2022

A set of variously substituted 1-arylpyrazol-3-one derivatives, including the di-ortho-aryl substituted ones, was synthesized as new potential anticancer compounds. To fulfill this aim, herein a regiospecific synthesis was proposed utilizing a new revisited one pot procedure, starting from commercial anilines and easily accessible 2,5-dimethyl-furan-3-one. In the course of the sequential ordered steps, in some cases, a nitro group displacement by chlorine took place to a minor extent. The in vitro screening against the full panel of ~60 human cancer cell lines (NCI) showed a moderate, but promising selective antiproliferative activity against the UO31 renal tumor cell line, only in compound…

The role of side chains in Substituted Pyrrole derivatives towards antiproliferative activity

2014

In the last years, the introduction of side chains in different molecular compounds takes increasing importance. As recently reported in literature, heterocyclic scaffolds with poor biological activity , if properly decorated with selected side chains, can improve their anticancer activity against a large spectrum of human tumor cell lines. For example, the annelated Pyrrolo[3,4-e]Pyrimidines and Pyrrolo[3,2-e]Pyrimidines, opportunely functionalized with a large number of side chains, showed a good increase in the antitumor activity with respect to the starting core structure. New compound thus obtained showed antiproliferative activity against all the human tumor cells, generally in the lo…

Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole derivatives: as anticancer and antibiofilm agents, and preclinical invest…

2020

Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

2016

New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S ph…

Correlation between cell line chemosensitivity and protein expression pattern as new approach for the design of targeted anticancer small molecules

2022

BACKGROUND AND RATIONALE: Over the past few decades, several databases with a significant amount of biological data related to cancer cells and anticancer agents (e.g.: National Cancer Institute database, NCI; Cancer Cell Line Encyclopedia, CCLE; Genomic and Drug Sensitivity in Cancer portal, GDSC) have been developed. The huge amount of heterogeneous biological data extractable from these databanks (among all, drug response and protein expression) provides a real foundation for predictive cancer chemogenomics, which aims to investigate the relationships between genomic traits and the response of cancer cells to drug treatment with the aim to identify novel therapeutic molecules and targets…

Synthesis of the New Ring System Bispyrido[4',3':4,5]pyrrolo [1,2-a:1',2'-d]pyrazine and Its Deaza Analogue

2014

Derivatives of the new ring systems bispyrido[4',3':4,5]pyrrolo[1,2-a:1',2'-d] pyrazine-6,13-dione and its deaza analogue pyrido[4'',3'':4',5']pyrrolo-[1',2':4,5]pyrazino [1,2-a]indole-6,13-dione were conveniently synthesized through a four-step sequence. Symmetrical derivatives of the former ring system were obtained through self condensation. On the other hand, condensation of 6-azaindole carboxylic acid with indole 2-carboxylic acid afforded the deaza analogue ring system. Derivatives of the title ring system were tested by the National Cancer Institute (Bethesda, MD, USA) and four of them exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cel…

Photochemotherapeutic haterocyclic agents having antiproliferative and antineoplastic activity

2011

Antiproliferative activity of Pyrrolo[3,2-c]quinoline derivatives

2012

The pyrrolo[3,2-c]quinoline scaffold has been known as a core structure of a wide number of bioactive molecules. Several derivatives of such a tricyclic angular heterocycle have shown a wide spectrum of biological activities, such as hypotensive, anti-inflammatory properties, gastric (H)ATPase inhibition effect, and remarkable antitumor activity (1). The high therapeutic potentiality of such a skeleton along with our interest in targets featuring aza-polycondensed aromatic structures, attracted us to develop an alternative synthetic strategy, in order to reach a series of pyrrolo[3,2-c]quinolines in quantitative yields (2). The reaction of 3-acetyl-1,4-dione 1 with selected amines allowed th…

Bioactive compounds containing benzoxadiazole, benzothiadiazole, benzotriazole.

2010

Essential oil from the aerial parts of Centaurea cuneifolia Sibth. & Sm. and C. euxina Velen., two species growing wild in Bulgaria

2009

Abstract The volatile constituents of the aerial parts of Centaurea cuneifolia Sibth. & Sm. and Centaurea euxina Velen. from Bulgaria were extracted by hydrodistillation and were analyzed. The main components in C. cuneifolia were β-eudesmol (26.5%) and hexadecanoic acid (17.6%). The main components in C. euxina were hexadecanoic acid (20.3%), spathulenol (10.8%) and caryophyllene oxide (6.2%). The chemotaxonomic significances with respect to other previously studied species of the same sections ( Achrolopus and Phalolepis , respectively) are discussed.