Pd-catalyzed isocyanide insertion/nucleophilic attack by indole C-3/desulfonylation in the same pot: a direct access to indoloquinolines of pharmacological interest

RSC Advances ◽  
2015 ◽  
Vol 5 (77) ◽  
pp. 62966-62970 ◽  
Author(s):  
Bagineni Prasad ◽  
Suresh Babu Nallapati ◽  
Sunder Kumar Kolli ◽  
Atul Kumar Sharma ◽  
Swapna Yellanki ◽  
...  
Keyword(s):  
Small Molecules ◽  
Cascade Reaction ◽  
Cytotoxic Agents ◽  
Direct Access ◽  
Nucleophilic Attack ◽  
Pharmacological Interest

A Pd-catalyzed new cascade reaction furnished indoloquinolin based small molecules as potential cytotoxic agents.

ChemInform Abstract: Pd-Catalyzed Isocyanide Insertion/Nucleophilic Attack by Indole C-3/Desulfonylation in the Same Pot: A Direct Access to Indoloquinolines of Pharmacological Interest.

ChemInform ◽  
2015 ◽  
Vol 46 (49) ◽  
pp. no-no
Author(s):  
Bagineni Prasad ◽  
Suresh Babu Nallapati ◽  
Sunder Kumar Kolli ◽  
Atul Kumar Sharma ◽  
Swapna Yellanki ◽  
...  
Keyword(s):  
Direct Access ◽  
Nucleophilic Attack ◽  
Pharmacological Interest

scholarly journals Synthetic Heterocyclic Derivatives as Kinase Inhibitors Tested for the Treatment of Neuroblastoma

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7069
Author(s):  
Francesca Musumeci ◽  
Annarita Cianciusi ◽  
Ilaria D’Agostino ◽  
Giancarlo Grossi ◽  
Anna Carbone ◽  
...  
Keyword(s):  
Small Molecules ◽  
Pediatric Cancer ◽  
Kinase Inhibitors ◽  
Severe Disease ◽  
Chemotherapeutic Agents ◽  
Cytotoxic Agents ◽  
Specific Mechanism ◽  
Drug Candidates ◽  
Heterocyclic Derivatives ◽  
Tumor In Childhood

In the last few years, small molecules endowed with different heterocyclic scaffolds have been developed as kinase inhibitors. Some of them are being tested at preclinical or clinical levels for the potential treatment of neuroblastoma (NB). This disease is the most common extracranial solid tumor in childhood and is responsible for 10% to 15% of pediatric cancer deaths. Despite the availability of some treatments, including the use of very toxic cytotoxic chemotherapeutic agents, high-risk (HR)-NB patients still have a poor prognosis and a survival rate below 50%. For these reasons, new pharmacological options are urgently needed. This review focuses on synthetic heterocyclic compounds published in the last five years, which showed at least some activity on this severe disease and act as kinase inhibitors. The specific mechanism of action, selectivity, and biological activity of these drug candidates are described, when established. Moreover, the most remarkable clinical trials are reported. Importantly, kinase inhibitors approved for other diseases have shown to be active and endowed with lower toxicity compared to conventional cytotoxic agents. The data collected in this article can be particularly useful for the researchers working in this area.

A bifunctional pyrazolone–chromone synthon directed organocatalytic double Michael cascade reaction: forging five stereocenters in structurally diverse hexahydroxanthones

2019 ◽  
Vol 6 (9) ◽  
pp. 1485-1490 ◽  
Author(s):  
Xiong-Li Liu ◽  
Xiong Zuo ◽  
Jun-Xin Wang ◽  
Shun-qin Chang ◽  
Qi-Di Wei ◽  
...  
Keyword(s):  
Small Molecules ◽  
Natural Product ◽  
Cascade Reaction

The merging of two or more known natural product-based scaffolds is a powerful and routine strategy to develop bioactive small molecules.

AlCl3-mediated hydroarylation–heteroarylation in a single pot: a direct access to densely functionalized olefins of pharmacological interest

2013 ◽  
Vol 49 (56) ◽  
pp. 6268 ◽  
Author(s):  
Ali Nakhi ◽  
Sivakumar Archana ◽  
Guru Pavan Kumar Seerapu ◽  
Keerthana Sarma Chennubhotla ◽  
Kummari Lalith Kumar ◽  
...  
Keyword(s):  
Direct Access ◽  
Pharmacological Interest

ChemInform Abstract: Creation of Molecular Complexities via a New Cu-Catalyzed Cascade Reaction: A Direct Access to Novel 2,2′-Spirobiindole Derivatives.

ChemInform ◽  
2015 ◽  
Vol 46 (24) ◽  
pp. no-no
Author(s):  
Bagineni Prasad ◽  
Raju Adepu ◽  
Atul Kumar Sharma ◽  
Manojit Pal
Keyword(s):  
Cascade Reaction ◽  
Direct Access

ChemInform Abstract: AlCl3-Mediated Hydroarylation-Heteroarylation in a Single Pot: A Direct Access to Densely Functionalized Olefins of Pharmacological Interest.

ChemInform ◽  
2013 ◽  
Vol 44 (43) ◽  
pp. no-no
Author(s):  
Ali Nakhi ◽  
Sivakumar Archana ◽  
Guru Pavan Kumar Seerapu ◽  
Keerthana Sarma Chennubhotla ◽  
Kummari Lalith Kumar ◽  
...  
Keyword(s):  
Direct Access ◽  
Pharmacological Interest

Synthesis of 2-substituted Furo[3,2-b]pyridines Under Pd/C-Cu Catalysis Assisted by Ultrasound: Their Evaluation as Potential Cytotoxic Agents

2020 ◽  
Vol 20 (8) ◽  
pp. 932-940 ◽  
Author(s):  
Dandamudi Sri Laxmi ◽  
Suryadevara V. Vardhini ◽  
Venkata R. Guttikonda ◽  
Mandava V.B. Rao ◽  
Manojit Pal
Keyword(s):  
Cell Lines ◽  
Ultrasound Irradiation ◽  
Cytotoxic Agents ◽  
Direct Access ◽  
Pyridine Derivative ◽  
Anticancer Activities ◽  
One Pot ◽  
Anticancer Properties ◽  
Mcf 7

Background: Compounds containing furo[3,2-b]pyridine framework have shown interesting pharmacological properties, including anticancer activities. Though these compounds are generally synthesized via the heteroannulation processes involving acetylenic derivatives, some of them are complex. Objective: The study aimed to explore a series of 2-substituted furo[3,2-b]pyridines for their cytotoxic properties against cancer cell lines in vitro. Methods: We developed a convenient synthesis of 2-substituted furo[3,2-b]pyridines via sequential (i) C-C coupling followed by (ii) C-O bond-forming reactions in a single pot. The reactions were performed under ultrasound irradiation in the presence of Pd/C as an inexpensive, stable and widely used catalyst. A range of 2- substituted furo[3,2-b]pyridines were synthesized via coupling of 3-chloro-2-hydroxy pyridine with terminal alkynes in the presence of 10% Pd/C-CuI-PPh3-Et3N in EtOH. The in vitro evaluation of all these compounds was carried out against MDA-MB-231 and MCF-7 cell lines and subsequently against SIRT1. Results: The furo[3,2-b]pyridine derivative 3b showed encouraging growth inhibition of both MDAMB-231 and MCF-7 cell lines and inhibition of SIRT1. The compound 3b also showed apoptosis-inducing potential when tested against MCF-7 cells. Conclusion: The Pd/C-Cu catalysis under ultrasound accomplished a one-pot and direct access to 2-substituted furo[3,2-b]pyridine derivatives, some of which showed anticancer properties.

Uncatalyzed CO2Li-Mediated SNAr Reaction of Unprotected Benzoic Acids via Silicon Trickery

2016 ◽  
Vol 69 (3) ◽  
pp. 307 ◽  
Author(s):  
Mickael Belaud-Rotureau ◽  
Anne-Sophie Castanet ◽  
Thi Huu Nguyen ◽  
Jacques Mortier
Keyword(s):  
Methoxy Group ◽  
Intermediate Formation ◽  
Coupling Reaction ◽  
Nucleophilic Aromatic Substitution ◽  
Direct Access ◽  
Nucleophilic Attack ◽  
Benzoic Acids ◽  
Aromatic Substitution ◽  
Snar Reaction ◽  
Ketone Formation

The alkyl and aryllithium nucleophilic aromatic substitution (SNAr) displacement of a fluoro or methoxy group from unprotected 2-fluoro/methoxybenzoic acids is discussed. It was discovered that a TMS group located at the C6-position ortho to the carboxyl group shields effectively the carboxylate against nucleophilic attack, thus reducing dramatically ketone formation, and reorients nucleophilic substitution to the C2-position. The reactions with fluoro-substituted substrate 7 proceed efficiently; in contrast, the use of methoxy-functionalized benzoic acid 8 only affords moderate yields with s-BuLi and PhLi. This uncatalyzed coupling reaction, which provides a direct access to biaryl compounds, presumably proceeds by an addition–elimination sequence via intermediate formation of a resonance-stabilized pentavalent silalactone-Meisenheimer complex.

scholarly journals Pseudoprogression in lung cancer: a case report

2020 ◽  
Vol 1 (5) ◽  
Author(s):  
Giulia Meoni ◽  
Nicola Libertà Decarli ◽  
Maurizio Benucci ◽  
Claudio Raspanti ◽  
Angela Stefania Ribecco
Keyword(s):  
Lung Cancer ◽  
Small Molecules ◽  
Response Pattern ◽  
Tumor Response ◽  
Checkpoint Inhibitors ◽  
Performance Status ◽  
Inflammatory Cells ◽  
Tumor Burden ◽  
Cytotoxic Agents ◽  
Lung Adenocarcinoma Patient

Immunotherapy dramatically changed the management of several malignancies including non-small cell lung cancer (NSCLC). Since immune checkpoint inhibitors have a different mechanism of action from cytotoxic agents or small molecules against NSCLC, also tumor response may present with atypical features. Pseudoprogression (PP) is a distinct response pattern defined by a transient enlargement of the tumor burden, sustained by inflammatory cells and usually not associated with worsening of performance status (PS). Here the authors describe the case of a lung adenocarcinoma patient treated with pembrolizumab, who developed an early symptomatic PP with a dramatic global worsening of PS. Subsequently an improvement in general condition and a brilliant tumor response were observed. Tumor re-biopsy was collected after the treatment in order to support the identification of PP and to describe microenvironment modifications induce by immunotherapy.

scholarly journals Palladium catalysed, three-component cascade reaction for the efficient synthesis of diverse small molecules

2020 ◽  
Vol 61 (46) ◽  
pp. 152536
Author(s):  
Jack Herbert ◽  
Kelsey Edwards ◽  
Visuvanathar Sridharan
Keyword(s):  
Small Molecules ◽  
Cascade Reaction ◽  
Efficient Synthesis
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