Delving into the Latest Updates on Centro Atlántico del Medicamento, S.A. with Synapse

Overview

Tags

Neoplasms

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	1

Top 5 Drug Type	Count

Small molecule drug	1

Top 5 Target	Count

ERα(Estrogen receptor alpha)	1

The naphthoquinone moiety is commonly found in numerous natural cytotoxic compounds with diverse and pleiotropic modes of action (MOAs). The moiety can exist as a standalone pharmacophore or combined with other pharmacophores to enrich their MOAs. Here, we report that the synthetic fusion of naphthoquinones and oxazepines provides potent cytotoxic compounds with diverse MOAs. Fused oxazepine-naphthoquinones were identified through a cytotoxic screen in Saccharomyces cerevisiae. The two most active compounds, CM-568 and CM-728, contained the same 3-pyridyl appendage in the oxazepine ring and were further evaluated along with close chemical derivatives. Both were highly cytotoxic, killing yeast cells in the low micromolar range; however, the role of reactive oxygen species in their MOA was significantly different. Investigations with yeast strains specifically designed to assess cell cycle, chromatin compaction, and nucleolar activity suggest that at lethal concentrations, cells die shortly after drug exposure through programmed death. Conversely, at sublethal concentrations, cell cycle progression is severely impaired. Interestingly, CM-568 labels cells with highly refractive non-fluorescent parallel rods. We conclude that the oxazepine moiety confers novel cytotoxic MOAs to naphthoquinones, which may be potentially useful in pharmacology.

23 Apr 2024·ACS Omega

Biological Activity of 6,7-Dehydroxyroyleanone and Derivatives Obtained from Plectranthus aliciae (Codd) A.J.Paton

Article

Author: Nikolić, Milan ; Capote, Natalia A. ; Filipović, Nenad ; Domínguez-Martín, Eva M. ; Mandim, Filipa ; Teixidó-Trujillo, Silvia ; Figueiredo, Ana Cristina ; Barros, Lillian ; Rijo, Patrícia ; Díaz-Lanza, Ana M. ; Melgar, Bruno ; Pires, Tânia C. S. P. ; Finimundy, Tiane C. ; Filipe, Márcia S. ; Pereira, Raquel ; Isca, Vera M. S.

The Plectranthus genus (Lamiaceae) is known to be rich in abietane diterpenes. The bioactive 6,7-dehydroxyroyleanone (DHR, 1) was previously isolated from Plectranthus madagascariensis var. madagascariensis and var. aliciae. This study aimed to explore the occurrence of DHR, 1, in P. aliciae and the potential bioactivities of new semisynthetic derivatives from DHR, 1. Several extraction methods were evaluated, and the hydrodistillation, using a Clevenger apparatus, afforded the highest yield (77.8 mg/g of 1 in the essential oil). Three new acyl derivatives (2-4) were successfully prepared from 1 (yields of 86-95%). Compounds 1-4 showed antioxidant activity, antibacterial effects, potent cytotoxic activity against several cell lines, and enhanced anti-inflammatory activity that surpassed dexamethasone (positive control). These findings encourage further exploration of derivatives 2-4 for potential mechanisms of antitumoral, antioxidant, and anti-inflammatory capabilities, studying both safety and efficacy.

01 Jan 2023·International journal of biological sciences

Chemical-proteomics Identify Peroxiredoxin-1 as an Actionable Target in Triple-negative Breast Cancer

Article

Author: Díaz-Chico, Juan Carlos ; Díaz-Chico, Bonifacio Nicolás ; Guerra, Borja ; Del Rosario, Henoc ; Jiménez-Monzón, Roberto ; Quintana, José ; Spínola-Lasso, Elena ; Estévez, Francisco ; Montero, Juan Carlos ; Fernández-Pérez, Leandro ; McNaughton-Smith, Grant ; López, Manuel Rodríguez ; León, Francisco ; Pandiella, Atanasio ; Elokely, Khaled M

Triple-neg. breast cancer (TNBC) is difficult to treat; therefore, the development of drugs directed against its oncogenic vulnerabilities is a desirable goal.Herein, we report the antitumor effects of CM728, a novel quinone-fused oxazepine, against this malignancy. CM728 potently inhibited TNBC cell viability and decreased the growth of MDA-MB-231-induced orthotopic tumors.Furthermore, CM728 exerted a strong synergistic antiproliferative effect with docetaxel in vitro and this combination was more effective than the individual treatments in vivo.Chem. proteomic approaches revealed that CM728 bound to peroxiredoxin-1 (Prdx1), thereby inducing its oxidationMol. docking corroborated these findings. CM728 induced oxidative stress and a multi-signal response, including JNK/p38 MAPK activation and STAT3 inhibition.Interestingly, Prdx1 downregulation mimicked these effects. Finally, CM728 led to DNA damage, cell cycle blockage at the S and G2/M phases, and the activation of caspase-dependent apoptosis.Taken together, our results identify a novel compound with antitumoral properties against TNBC.In addition, we describe the mechanism of action of this drug and provide a rationale for the use of Prdx1 inhibitors, such as CM728, alone or in combination with other drugs, for the treatment of TNBC.

100 Deals associated with Centro Atlántico del Medicamento, S.A.

Login to view more data

100 Translational Medicine associated with Centro Atlántico del Medicamento, S.A.

Login to view more data

Corporation Tree

Boost your research with our corporation tree data.

login

or

view full example data

Boost your research with our corporation tree data.

Pipeline

Pipeline Snapshot as of 17 Jun 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

1

4

Other

Login to view more data

Current Projects

Drug(Targets)	Indications	Global Highest Phase

SERMs(CEAMED) ( ERα )	Neoplasms More	Preclinical
CM-801 ( BET )	Neoplasms More	Pending
CM-728 ( STAT3 )	Breast Cancer More	Pending
CM-363 ( STAT3 x STAT5 transcription factor )	Breast Cancer More	Pending
CM-681 ( STAT3 )	Neoplasms More	Pending